Original Pharmacodynamic and pharmacokinetic effects of S086, a novel angiotensin receptor neprilysin inhibitor
文献类型：期刊论文
| 作者 | Sun, Jingchao1; Xu, Wenjie1; Hua, Huaijie1; Xiao, Ying1; Chen, Xiaoyan2 ; Gao, Zhiwei2; Li, Song1; Jing, Xiaolong1; Du, Frank3; Sun, Guofeng3
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| 刊名 | BIOMEDICINE & PHARMACOTHERAPY
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| 出版日期 | 2020-09-01 |
| 卷号 | 129页码:10 |
| 关键词 | Angiotensin receptor-NEP inhibitor Heart failure Neprilysin inhibitor Angiotensin receptor blocker |
| ISSN号 | 0753-3322 |
| DOI | 10.1016/j.biopha.2020.110410 |
| 通讯作者 | Sun, Jingchao(sunjingchao@salubris.com) |
| 英文摘要 | Background and Purpose: Angiotensin receptor-NEP inhibitor (ARNi), which includes an angiotensin receptor blocker (ARB) and a neprilysin inhibitor (NEPi), has been proven safe and effective for treating heart failure with reduced ejection fraction (HF-REF). S086 is a novel single-molecule ARNi that includes the molecular moieties of Eo3174 (the active metabolite of the ARB losartan) and sacubitril (a NEP inhibitor prodrug) in a 1:1 M ratio. We performed preclinical animal model studies to evaluate the efficacy of S086 in treating HF. Experimental Approach: Rat and dog models of myocardial ischemia-induced chronic heart failure were used in this research. Principal Results: The oral administration of S086 dose-dependently lowered the heart weight index, attenuated cardiac fibrosis, and improved left ventricular ejection fraction, shortening fraction, and cardiac output, without effects on hemodynamics in animal models of myocardial ischemia-induced chronic heart failure. A comparable protective effect to LCZ696 was observed for S086 at an equal molar dose in dog models. In addition, S086 was superior to LCZ696 since it significantly reversed the decrease in left ventricular posterior wall end-systolic thickness. Conclusion: This animal study suggests that S086 is effective in treating myocardial ischemia-induced chronic heart failure. |
| WOS关键词 | HEART-FAILURE ; NATRIURETIC PEPTIDES ; ENALAPRIL ; HYPERTENSION ; METABOLITE ; VALSARTAN ; UPDATE |
| WOS研究方向 | Research & Experimental Medicine ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000566378900002 |
| 出版者 | ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/291580]  |
| 专题 | 中国科学院上海药物研究所 |
| 通讯作者 | Sun, Jingchao |
| 作者单位 | 1.Shenzhen Salubris Pharmaceut Co Ltd, 1 Feng Huang Gang Hua Bao Ind Dist, Shenzhen 518040, Guangdong, Peoples R China 2.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai, Peoples R China 3.WuXi AppTec Shanghai Co Ltd, Shanghai, Peoples R China |
| 推荐引用方式 GB/T 7714 | Sun, Jingchao,Xu, Wenjie,Hua, Huaijie,et al. Original Pharmacodynamic and pharmacokinetic effects of S086, a novel angiotensin receptor neprilysin inhibitor[J]. BIOMEDICINE & PHARMACOTHERAPY,2020,129:10. |
| APA | Sun, Jingchao.,Xu, Wenjie.,Hua, Huaijie.,Xiao, Ying.,Chen, Xiaoyan.,...&Sun, Guofeng.(2020).Original Pharmacodynamic and pharmacokinetic effects of S086, a novel angiotensin receptor neprilysin inhibitor.BIOMEDICINE & PHARMACOTHERAPY,129,10. |
| MLA | Sun, Jingchao,et al."Original Pharmacodynamic and pharmacokinetic effects of S086, a novel angiotensin receptor neprilysin inhibitor".BIOMEDICINE & PHARMACOTHERAPY 129(2020):10. |
入库方式： OAI收割
来源：上海药物研究所
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